Discovery of XL01126: a potent, fast, cooperative, selective, orally bioavailable, and blood–brain barrier penetrant PROTAC degrader of leucine-rich repeat kinase 2

X Liu, AF Kalogeropulou, S Domingos… - Journal of the …, 2022 - ACS Publications
Leucine-rich repeat kinase 2 (LRRK2) is one of the most promising targets for Parkinson's
disease. LRRK2-targeting strategies have primarily focused on type 1 kinase inhibitors …

Phosphoproteomics: a valuable tool for uncovering molecular signaling in cancer cells

JS Gerritsen, FM White - Expert review of proteomics, 2021 - Taylor & Francis
Introduction Many pathologies, including cancer, have been associated with aberrant
phosphorylation-mediated signaling networks that drive altered cell proliferation, migration …

CURTAIN—A unique web-based tool for exploration and sharing of MS-based proteomics data

TK Phung, K Berndsen, R Shastry… - Proceedings of the …, 2024 - National Acad Sciences
To facilitate analysis and sharing of mass spectrometry (MS)-based proteomics data, we
created online tools called CURTAIN (https://curtain. proteo. info) and CURTAIN-PTM …

Phosphoproteomic Approaches for Identifying Phosphatase and Kinase Substrates

AG DeMarco, MC Hall - Molecules, 2023 - mdpi.com
Protein phosphorylation is a ubiquitous post-translational modification controlled by the
opposing activities of protein kinases and phosphatases, which regulate diverse biological …

Design and characterization of SGK3-PROTAC1, an isoform specific SGK3 kinase PROTAC degrader

H Tovell, A Testa, H Zhou, N Shpiro… - ACS Chemical …, 2019 - ACS Publications
SGK3 is a PX domain containing protein kinase activated at endosomes downstream of
class 1 and 3 PI3K family members by growth factors and oncogenic mutations. SGK3 plays …

Development of a multiplexed targeted mass spectrometry assay for LRRK2-phosphorylated Rabs and Ser910/Ser935 biomarker sites

RS Nirujogi, F Tonelli, M Taylor, P Lis… - Biochemical …, 2021 - portlandpress.com
Mutations that increase the protein kinase activity of LRRK2 are one of the most common
causes of familial Parkinson's disease. LRRK2 phosphorylates a subset of Rab GTPases …

Molecular basis for the recruitment of the Rab effector protein WDR44 by the GTPase Rab11

MC Thibodeau, NJ Harris, ML Jenkins… - Journal of Biological …, 2023 - ASBMB
The formation of complexes between Rab11 and its effectors regulates multiple aspects of
membrane trafficking, including recycling and ciliogenesis. WD repeat–containing protein 44 …

Syntaxin 12 and COMMD3 are new factors that function with VPS33B in the biogenesis of platelet α-granules

AL Ambrosio, HP Febvre… - Blood, The Journal of the …, 2022 - ashpublications.org
Platelet α-granules regulate hemostasis and myriad other physiological processes, but their
biogenesis is unclear. Mutations in only 3 proteins are known to cause α-granule defects …

An eco-friendly, low-cost, and automated strategy for phosphoproteome profiling

W Zhang, CK Lai, W Huang, W Li, S Wu, Q Kong… - Green …, 2022 - pubs.rsc.org
Reversible protein phosphorylation plays a vital role in many biological processes. In current
phosphoproteomics, targeted enrichment before mass spectrometry (MS) analysis is …

In vitro reconstitution of Sgk3 activation by phosphatidylinositol 3-phosphate

D Pokorny, L Truebestein, KD Fleming, JE Burke… - Journal of Biological …, 2021 - ASBMB
Serum-and glucocorticoid-regulated kinase 3 (Sgk3) is a serine/threonine protein kinase
activated by the phospholipid phosphatidylinositol 3-phosphate (PI3P) downstream of …